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vorinostat + pegylated liposomal doxorubicin
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Nanoparticles → Drug Delivery Systems, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
vorinostat + pegylated liposomal doxorubicin is a combination chemotherapy regimen investigated by Yale University for the treatment of relapsed or refractory lymphomas. Vorinostat (Zolinza) is an orally bioavailable small molecule inhibitor of histone deacetylases (HDACs), specifically classes I and II. By inhibiting HDACs, vorinostat promotes the accumulation of acetylated histones, leading to chromatin remodeling and increased DNA accessibility. Pegylated liposomal doxorubicin (Doxil) is a nanoparticle formulation of the anthracycline doxorubicin, which acts by intercalating into DNA and inhibiting topoisomerase II, resulting in double-strand breaks and apoptosis. The combination is designed to exploit the synergistic potential of HDAC inhibition to sensitize cancer cells to the DNA-damaging effects of doxorubicin, a strategy supported by preclinical models showing enhanced cytotoxicity when these agents are used together.
- Brand names
- ZolinzaDoxilCaelyx
- Other names
- vorinostat + DoxilSAHA + PLDvorinostat + pegylated liposomal doxorubicin
02
Targets
TOP2A (DNA topoisomerase II)
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